Chitosan-coated nano-liposomes for the oral delivery of berberine hydrochloride

Nguyen, Thanh X.; Huang, Lin; Liu, Li; Abdalla, Ahmed M. E.; Gauthier, Mario; Yang, Guang

doi:10.1039/c4tb00876f

Cited by 120 publications

(95 citation statements)

References 57 publications

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“…The DLS‐based size analysis confirmed that the mean droplet size of RPG‐NEs was in the ideal nanometer range of 86.5 ± 3.4 nm, with a relatively narrow particle size distribution (PDI < 0.20) suggesting that the developed NEs were suitable as carriers for oral drug delivery goals (Figure a) (Awasthi et al, ; Nguyen et al, ). In addition, RPG‐NEs revealed negative ZP values of −33.2 ± 2.6 mV, implying a sufficiently high negative surface charge assuring the enough repulsive forces between the oil droplets which, in turn, prevent any kind of breaking or coalescence, thus leading to a highly stable NE (Elsheikh et al, ).…”

Section: Discussionmentioning

confidence: 76%

“…P188 is frequently used in pharmaceutical formulations as emulsifying, solubilizing, and dispersing agents, as well as absorbance enhancer (Hillery & Florence, 1996;Zhuang et al, 2010). Pluronics and polysorbates have been reported to increase the permeability of various drugs both in vitro and in vivo (Azmin et al, 1982;Zhang, Yao, Morrison, & Chong, 2003 Figure 2a) (Awasthi et al, 2003;Nguyen et al, 2014). In addition, RPG-NEs revealed negative ZP values of −33.2 ± 2.6 mV, implying a sufficiently high negative surface charge assuring the enough repulsive forces between the oil droplets which, in turn, prevent any kind of breaking or coalescence, thus leading to a highly stable NE (Elsheikh et al, 2012).…”

Section: Discussionmentioning

confidence: 99%

“…As well, chitosan (Cs), a natural positively charged polysaccharide, is frequently used to modify the physicochemical property of various drug delivery systems. Surface coating with chitosan can improve the stability of nanocarriers in various biological fluids including simulated gastric fluid (SGF) and intestinal fluid (SIF), as well as their mucoadhesive properties, cellular uptake, and ultimately drug absorption (Kawashima, Yamamoto, Takeuchi, & Kuno, ; Nguyen et al, ).…”

Section: Introductionmentioning

confidence: 99%

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Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

et al. 2019

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The aim of the present study was to develop modified nanoemulsions to improve the oral bioavailability and pharmacokinetics of a poor water‐soluble drug, repaglinide (RPG). The repaglinide‐loaded nanoemulsions (RPG‐NEs) were prepared from olive oil as internal phase, span 80, tween 80, and poloxamer 188 as emulsifiers, using homogenization technique. The mean droplet size, zeta potential, and entrapment efficiency of RPG‐NEs were 86.5 ± 3.4 nm, −33.8 ± 2.1 mV, and 96.3 ± 2.3%, respectively. The chitosan‐coated RPG‐NEs (Cs‐RPG‐NEs) showed an average droplet size of 149.3 ± 3.9 nm and a positive zeta‐potential of +31.5 ± 2.8 mV. Drug release profile of RPG‐NEs was significantly higher than free drug in the simulated gastrointestinal fluids (p < .005). The in vivo study revealed 3.51‐ and 1.78‐fold increase in the AUC0‐12h and Cmax of the drug, respectively, in RPG‐NEs‐receiving animals in comparison to the free drug. The pharmacokinetic analysis confirmed that Cs‐RPG‐NEs were more efficient than uncoated ones for the oral delivery of RPG. Cs‐RPG‐NEs showed a longer t1/2 and higher AUC0‐∞ compared to control group. The relative bioavailability of Cs‐RPG‐NEs was higher than that of uncoated RPG‐NEs and free drug. Collectively, these findings suggest that chitosan‐coated nanoemulsions are promising carrier for improving the oral bioavailability of RPG.

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Section: Discussionmentioning

confidence: 76%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

et al. 2019

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“…The results indicated enhanced cytotoxicity in comparison to free berberine (Wen et al, 2011; Lin et al, 2014; Sailor et al, 2015). …”

Section: Liposomesmentioning

confidence: 95%

PhytoNanotechnology: Enhancing Delivery of Plant Based Anti-cancer Drugs

2018

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Natural resources continue to be an invaluable source of new, novel chemical entities of therapeutic utility due to the vast structural diversity observed in them. The quest for new and better drugs has witnessed an upsurge in exploring and harnessing nature especially for discovery of antimicrobial, antidiabetic, and anticancer agents. Nature has historically provide us with potent anticancer agents which include vinca alkaloids [vincristine (VCR), vinblastine, vindesine, vinorelbine], taxanes [paclitaxel (PTX), docetaxel], podophyllotoxin and its derivatives [etoposide (ETP), teniposide], camptothecin (CPT) and its derivatives (topotecan, irinotecan), anthracyclines (doxorubicin, daunorubicin, epirubicin, idarubicin), and others. In fact, half of all the anti-cancer drugs approved internationally are either natural products or their derivatives and were developed on the basis of knowledge gained from small molecules or macromolecules that exist in nature. Three new anti-cancer drugs introduced in 2007, viz. trabectedin, epothilone derivative ixabepilone, and temsirolimus were obtained from microbial sources. Selective drug targeting is the need of the current therapeutic regimens for increased activity on cancer cells and reduced toxicity to normal cells. Nanotechnology driven modified drugs and drug delivery systems are being developed and introduced in the market for better cancer treatment and management with good results. The use of nanoparticulate drug carriers can resolve many challenges in drug delivery to the cancer cells that includes: improving drug solubility and stability, extending drug half-lives in the blood, reducing adverse effects in non-target organs, and concentrating drugs at the disease site. This review discusses the scientific ventures and explorations involving application of nanotechnology to some selected plant derived molecules. It presents a comprehensive review of formulation strategies of phytoconstituents in development of novel delivery systems like liposomes, functionalized nanoparticles (NPs), application of polymer conjugates, as illustrated in the graphical abstract along with their advantages over conventional drug delivery systems supported by enhanced biological activity in in vitro and in vivo anticancer assays.

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“…These liposomes can be coated with mucoadhesive polymers to increase the residence time at the ulcerated area. Some researchers have reported chitosan-coated liposomes can improve their properties and applicability 6 . First generation mucoadhesive polymers like chitosan, karaya gum etc.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Curcumin Loaded Thiolated Polymer Coated Liposomes for Aphthous Ulcers

Munot¹,

Gujar²

2019

Int. Res. J. Pharm.

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Aphthous ulcers or Recurrent Aphthous Stomatitis (RAS) are inflammatory lesions of mucous lining of mouth associated with redness, swelling and occasional bleeding from affected area(s). Curcumin, a herbal drug was selected due to its antioxidant, anti-inflammatory, antimicrobial and wound healing ability. Present study deals with formulation, optimization and evaluation of curcumin loaded liposomes for local drug delivery as liposomes have property to get concentrated in inflamed areas. Efficacy of liposomes was enhanced in terms of mucoadhesion, retention in the buccal mucosa and sustained release of drug by coating them with Thiolated Karaya gum. Curcumin loaded liposomes, prepared using thin film hydration method were optimized by 3 2 factorial design using Design Expert Software. Batch F8 having entrapment 75.1±0.94 % and controlled the release of curcumin up to 12 h was considered optimized and was coated with thiolated karaya gum to get TKF8. Successful coating was evident from TEM images, increase in particle size from 129.86 ± 9.1 nm to 152.39 ± 1.3 nm, zeta potential from negative to positive -10.5 mV to 9.55mV. TKF8 showed better mucoadhesion by absorbing 6.98 % more amount of mucin and also had ability to concentrate in the buccal mucosa for 24 h as observed using exvivo studies. It can be attributed to positively charged thiolated polymer interacting with negatively charged sialic acid residues in the mucus. Drug release from F8 and TKF8 was sustained for 12 h and 24 h respectively and they followed diffusion controlled release (Peppas model). This formulation can be efficient therapeutic strategy for apthous ulcers which would provide relief to the patients.

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Chitosan-coated nano-liposomes for the oral delivery of berberine hydrochloride

Abstract: Since desirable in vitro and in vivo characteristics were achieved, chitosan-coated nano-liposomes are promising release devices for the oral delivery of berberine hydrochloride increasing the bioavailability of the drug.

Cited by 120 publications

References 57 publications

Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

PhytoNanotechnology: Enhancing Delivery of Plant Based Anti-cancer Drugs

Formulation and Evaluation of Curcumin Loaded Thiolated Polymer Coated Liposomes for Aphthous Ulcers

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